Caspase

Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner.

Duocarmycin A, which is one of well-known antitumor antibiotics, is a DNA alkylator and efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results HLC-2 cells typically apoptotic changes, including chromatin condensation, sub-G1 accumulation in DNA histogram pattern, and decrease in procaspase-3 and 9 levels.

Emricasan is an orally active, irreversible, broad-spectrum caspase inhibitor with good pharmacokinetic profile.

Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation.

MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line.

Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii Maxim. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.

Phenoxodiol is an isoflavone derivative with antitumor activity.

Taurodeoxycholic acid sodium hydrate (Sodium taurodeoxycholate monohydrate), a bile acid, is an amphiphilic surfactant molecule synthesized from cholesterol in the liver. It activates S1PR2 pathway in addition to the TGR5 pathway.

Thevetiaflavone could upregulate the expression of Bcl?2 and downregulate that of Bax and caspase?3.

ZYZ-488 is a competitive apoptotic protease activating factor-1 (Apaf-1) inhibitor. ZYZ-488 inhibits the activation of binding protein procaspase-9 and procaspase-3.

Dehydrotrametenolic acid is a sterol isolated from the sclerotium of Poria cocos.

Ac-AAVALLPAVLLALLAP-IETD-CHO is a composite of Ac-IETD-CHO, a peptide inhibitor of caspase-8, and a cell-permeable hydrophobic sequence derived from K-FGF.

Ac-AAVALLPAVLLALLAP-DEVD-CHO is a composite of Ac-DEVD-CHO, a peptide inhibitor of caspase-3 and -7, and a cell-permeable hydrophobic sequence derived from K-FGF.

Ac-AAVALLPAVLLALLAP-VAD-CHO is a composite of Ac-VAD-CHO, a non-selective caspase inhibitor, and a cell-permeable hydrophobic sequence derived from K-FGF.

Z-VA-DL-D(OMe)-FMK (Z-VAD-FMK) is a pan-caspase inhibitor.

Boc-AEVD-CHO is an inhibitor of caspase-8 (Ki = 1.6 nM) that also inhibits caspase-1, -3, -6, and -9 (Kis = 10,000, 375, 438, 425, and 320 nM, respectively).

Ac-IETD-CHO (trifluoroacetate salt) is a caspase 8 inhibitor that can prevent the focal adhesion kinase (Fak) from being cleaved by caspase, with an IC 50 value of 200nM.

L-Sulforaphane is an orally active, non-specific activator of nuclear factor erythroid 2-related factor 2 (Nrf2), which functions by inhibiting the interaction between Keap1 protein and Nrf2.

Ac-DMQD-CHO is a peptide inhibitor of caspase-3 (IC50 = 39 nM).

Ac-LEVD-CHO is a caspase-4 inhibitor.

Ac-VDVAD-CHO is an inhibitor of caspase-2, -3, and -7 (Kis = 3.5, 1, and 7.5 nM, respectively).

Ac-VEID-CHO is an inhibitor of caspase-6 (IC50 = 16.2 nM).

Caspase-9 inhibitor III is an inhibitor of caspase-9 with cardioprotective effects.